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Niaprazine

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Niaprazine (INN) (aha aha Nopron) bụ ọgwụ na-eme ka mmadụ kwụsị ịlụ ọgụ nke otu phenylpiperazine.[1][2] A na-eji ya agwọ nsogbu ụra kemgbe mmalite afọ 1970 na ọtụtụ mba Europe nke ụwa gụnyere France, Italy, na Luxembourg.[3][4] A na-ejikarị ya eme ihe na ụmụaka hụrụ ndị ọzọ ụra na ndị nọ n'afọ iri na ụma n'ihi nchekwa ya dị mma na njirimara nnagide na enweghị ike mmetọ.[5][6][7][8][9][10]

Na mbụ, e kwenyere na ọ na-arụ ọrụ dị ka antihistamine na anticholinergic, e mechara chọpụta na niaprazine nwere njikọ dị ala ma ọ bụ enweghị njikọ maka ndị na-anabata H<sub id="mwMg">1</sub> na mACh (Ki = > 1 μM), ma chọpụta na ọ na ọ na'arụ ọrụ dị ike ma họrọ 5-HT2A na α1-adrenergic receptor antagonist (Ki = 75 nM na 86 nM, n'otu n'otu).[11][12] Ọ nwere obere ma ọ bụ enweghị njikọ nke ụwa na ụdị nke dị ka ndị na eme ka anyị maka 5-HT1A, 5-HT2B, D2, na β-adrenergic, yana na SERT na VMAT (Ki = niile > 1 μM), mana ọ nwere ụfọdụ njikọ maka onye na-anabata α2-adrenergics (Ki = 730 nM).[12]

E gosipụtara na Niaprazine na-agbanwe na para-fluorophenylpiperazine (pFPP) n'ụzọ yiri nke trazodone na nefazodone na-agbari na meta-chlorophenylpierazine (mCPP).[13][14] Ọ bụghị ihe doro anya ọrụ, ma ọ bụrụ na ọ dị, pFPP na-arụ na mmetụta ahụike nke niaprazine.[12] Otú ọ dị, site na ọmụmụ nke ụwa na ụdị ke amụta na anụmanụ a maara na pFPP, n'adịghị ka niaprazine, anaghị emepụta mmetụta sedative, kama ọ na-egosipụta njirimara omume na-egosi ọrụ serotonergic.[13]

Ntụaka

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  1. ↑ The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. 14 November 2014. pp. 862–. ISBN 978-1-4757-2085-3.
  2. ↑ Sleep: physiology, investigations, and medicine. New York: Kluwer Academic/Plenum. 2003. ISBN 978-0-306-47406-4.
  3. ↑ Swiss Pharmaceutical Society (2000). Index Nominum 2000: International Drug Directory (Book with CD-ROM). Boca Raton: Medpharm Scientific Publishers. ISBN 978-3-88763-075-1.
  4. ↑ Dictionary of Pharmacological Agents. Boca Raton: Chapman & Hall/CRC. 1996. ISBN 978-0-412-46630-4.
  5. ↑ "[Niaprazine in behavior disorders in children. Double-blind comparison with placebo]". La Pediatria Medica e Chirurgica: Medical and Surgical Pediatrics (in Italian). 9 (2): 185–7. 1987. PMID 2958783.
  6. ↑ "[Niaprazine and side effects in pediatrics. Cooperative evaluation of French centers of pharmacovigilance]". Thérapie (in French). 43 (4): 307–11. 1988. PMID 2903572.
  7. ↑ "The effect of niaprazine on some common sleep disorders in children. A double-blind clinical trial by means of continuous home-videorecorded sleep". Child's Nervous System. 7 (6): 332–5. October 1991. doi:10.1007/bf00304832. PMID 1837245.
  8. ↑ "Niaprazine vs chlordesmethyldiazepam in sleep disturbances in pediatric outpatients". Pharmacological Research. 25 Suppl 1: 83–4. 1992. doi:10.1016/1043-6618(92)90551-l. PMID 1354861.
  9. ↑ "Insomnia in children: when are hypnotics indicated?". Paediatric Drugs. 4 (6): 391–403. 2002. doi:10.2165/00128072-200204060-00006. PMID 12038875.
  10. ↑ "Anxiolytics, hypnotics, and antidepressants dispensed to adolescents in a French region in 2002". Pharmacoepidemiology and Drug Safety. 15 (7): 494–503. July 2006. doi:10.1002/pds.1258. PMID 16700077.
  11. ↑ "[Some pharmacodynamical properties of niaprazine, a new antihistaminic agent]". Thérapie (in French). 26 (6): 1203–9. 1971. PMID 4401719.
  12. 1 2 3 "Molecular pharmacology of niaprazine". Progress in Neuro-psychopharmacology & Biological Psychiatry. 12 (6): 989–1001. 1988. doi:10.1016/0278-5846(88)90093-0. PMID 2853885.
  13. 1 2 "The effect of niaprazine on the turnover of 5-hydroxytryptamine in the rat brain". Neuropharmacology. 21 (2): 163–9. February 1982. doi:10.1016/0028-3908(82)90157-5. PMID 6460945.
  14. ↑ "Critical notes on the specificity of drugs in the study of metabolism and functions of brain monoamines". International Review of Neurobiology. 29: 259–80. 1988. doi:10.1016/s0074-7742(08)60089-6. PMID 3042665.